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腹腔注射β-咔啉羧酸乙酯及其游离酸对小鼠体内地西泮和丙戊酸钠抗惊厥活性的影响。

The effects of beta-carboline carboxylic acid ethyl ester and its free acid, administered ICV, on the anticonvulsant activity of diazepam and sodium valproate in the mouse.

作者信息

Vellucci S V, Webster R A

出版信息

Pharmacol Biochem Behav. 1986 Apr;24(4):823-7. doi: 10.1016/0091-3057(86)90418-1.

DOI:10.1016/0091-3057(86)90418-1
PMID:3012595
Abstract

The effects of intracerebroventricular (ICV) beta-carboline carboxylic acid ethyl ester (beta-CCE) and its free acid on the protective effects of diazepam against leptazol- and R05-3663-induced convulsions were investigated in mice and compared with their effects on the antileptazol effect of sodium valproate, in an attempt to demonstrate a specific central effect of beta-CCE on benzodiazepine function. The results show that a small dose (1 microgram) of beta-CCE but not its free acid (in doses of up to 100 micrograms) was able to reverse the protective effects of diazepam against leptazol- and R05-3663-induced convulsions, whereas the effects of sodium valproate, a nonbenzodiazepine anticonvulsant, could not be reversed by these beta-carboline derivatives.

摘要

在小鼠中研究了脑室内注射β-咔啉羧酸乙酯(β-CCE)及其游离酸对安定抗戊四氮和R05-3663诱导惊厥的保护作用的影响,并将其与它们对丙戊酸钠抗戊四氮作用的影响进行比较,以试图证明β-CCE对苯二氮䓬功能的特定中枢作用。结果表明,小剂量(1微克)的β-CCE而非其游离酸(剂量高达100微克)能够逆转安定对戊四氮和R05-3663诱导惊厥的保护作用,而丙戊酸钠(一种非苯二氮䓬类抗惊厥药)的作用不能被这些β-咔啉衍生物逆转。

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